Journal Article10.1016/S0223-5234(01)01321-6
Synthesis, antiarrhythmic, and antihypertensive effects of novel 1-substituted pyrrolidin-2-one and pyrrolidine derivatives with adrenolytic activity.
Barbara Malawska,Katarzyna Kulig,Barbara Filipek,Jacek Sapa,Dorota Maciąg,Małgorzata Zygmunt,Lucyna Antkiewicz-Michaluk +6 more
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TL;DR: The pharmacological results and binding studies suggest that their antiarrhythmic and hypotensive effects may be related to their alpha-adrenolytic properties, and that those properties depend on the presence of the 1-phenylpiperazine moiety with a methoxy- or chloro- substituent in the ortho position in the phenyl ring.
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About: This article is published in European Journal of Medicinal Chemistry. The article was published on 01 Mar 2002. The article focuses on the topics: Pyrrolidine.
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Citations
Synthesis and evaluation of in vivo activity of diphenylhydantoin basic derivatives.
Tomasz Dylag,Małgorzata Zygmunt,Dorota Maciag,Jadwiga Handzlik,Marek Bednarski,Barbara Filipek,Katarzyna Kieć-Kononowicz +6 more
TL;DR: Water-soluble compounds, containing 2-methoxyphenylpiperazine group (11a, 19a), showed strong antiarrhythmic properties in adrenaline-induced arrhythmia; compound 9a {1-[3-(4-(3-chloro-phenyl)-piperazin-1-yl)- 2-hydroxy-propyl]- 3-ethyl-2,4-dioxo-5,5-diphenyl-
58
Synthesis, α1-adrenoceptor antagonist activity, and SAR study of novel arylpiperazine derivatives of phenytoin
Jadwiga Handzlik,Dorota Maciąg,Monika Kubacka,Szczepan Mogilski,Barbara Filipek,Katarzyna Stadnicka,Katarzyna Kieć-Kononowicz +6 more
TL;DR: Molecular modelling results obtained using conformational analysis CONFLEX and PM5 method for geometry optimization allowed for comparison of the spatial properties of tested compounds with pharmacophore model created by Barbaro et al. for the ideal alpha(1)-adrenoceptor antagonist.
49
Chemoenzymatic synthesis with lipase catalyzed resolution and evaluation of antitumor activity of (R/S)-2-[2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl]-1H-pyrrolo[3,4-b]quinolin-3(2H)-one.
TL;DR: Newly synthesized and resolved compounds were screened for their antitumor activity against cancer cells such as human neuroblastoma SK-N-SH and human lung carcinoma A549 cell line in vitro and showed that the compound 1 S-(-) alcohol was more effective in inhibiting the tumor cell growth.
48
Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone
Natalia Szkaradek,Anna Rapacz,Karolina Pytka,Barbara Filipek,Agata Siwek,Marek T. Cegla,Henryk Marona +6 more
TL;DR: Results were quite promising and suggested that in the group of xanthone derivatives new potential antiarrhythmics and hypotensives might be found.
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Synthesis and Pharmacological Evaluation of New 1-[3-(4-Arylpiperazin-1-yl)-2-hydroxypropyl]-pyrrolidin-2-one Derivatives with Anti-arrhythmic, Hypotensive, and α-Adrenolytic Activity
TL;DR: It was found that the presence of the piperazine ring and a hydroxy group in the second position of the propyl chain are critical structural features in determining the affinity of the compounds tested.
37
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In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia
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